Abstract

A series of polyphenolic-sulfonated compounds were observed to have potent anti-inflammatory activity
and were protective against induced endotoxic shock in mice at 8 and 16 mg/kg, I.P. These agents proved
to be potent elastase inhibitors in human leukocytes and J774-AI and IC-21 mouse macrophages as well as
prostaglandin cyclo-oxygenase inhibitors in J774-AI macrophages. The compounds from 5 to 50 μM
inhibited TNFα release from IC-21 macrophages and IL-1 release from mouse P388D1 macrophages
induced by LPS. The binding of these cytokines to high affinity receptors on target cells, e.g. L929
fibroblasts and IL-2 in HuT78 T lymphoma cells, were also suppressed by the agents. These compounds
blocked the adhesion of leukocytes and macrophages to the plasma membranes of L929 fibroblasts.